HET0016-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHET0016Cat.No.:HY-124527CASNo.:339068-25-6分⼦式:C₁₂H₁₈N₂O分⼦量:206.28作⽤靶点:CytochromeP450作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DCM:12.5mg/mL(60.60mM;Needultrasonic)DMSO:5mg/mL(24.24mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.8478mL24.2389mL48.4778mL5mM0.9696mL4.8478mL9.6956mL10mM0.4848mL2.4239mL4.8478mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：20%HP-β-CDinsaline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2mg/mL(9.70mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性HET0016⼀种⾼效、选择性的20-HETE合成酶抑制剂，对重组CYP4A1、CYP4A2和CYP4A3催化20-HETE合成作⽤的IC50值分别为17.7nM,12.1nM和20.6nM。HET0016⼀种选择性CYP450抑制剂，已被证明可以抑制⾎管⽣成和肿瘤⽣长[1][2]。IC50&Target17.7nM(CYP4A1),12.1nM(CYP4A2),20.6nM(CYP4A3)[1],CYP450[2]体外研究HET0016isaselective,non-competitiveandirreversibleinhibitorofCYP4A[1].HET0016(100μM;24hours,48hours)decreasesmigrationandinvasionofbreastcancermetastaticcells[2].CellProliferationAssay[2]CellLine:MDA-MB-231cellsConcentration:100μMIncubationTime:24hours,48hoursResult:Decreasedmigrationandinvasionofbreastcancermetastaticcells体内研究HET0016(10mg/kg/day;i.v.;for3weeks)reducestumorvolumeandlungmetastasisinanimmunocompetentbreastcancermousemodel[2].HET0016reducesthemetalloproteinases’levelsinthelungsviaPI3K/AKTpathwayinmice[2].HET0016decreasesexpressionofpro-inflammatoryandgrowthfactorsandgranulocyticMDSCspopulationinlungmicroenvironment[2].HET0016protectsBBBdysfunctionafterI/RbyregulatingtheexpressionofMMP-9andtightjunctionproteins[3].AnimalModel:4–5weeksfemaleBalb/cmice(16-18g)[2]Dosage:10mg/kg/dayAdministration:Intravenously;5daysaweek;for3weeks;startingfromday15oftumorimplantationResult:Reducedtumorvolumeandlungmetastasis.户使⽤本产品发表的科研⽂献•CellDeathDis.2022Jul28;13(7):653.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].SekiT,etal.CytochromeP4504AisoforminhibitoryprofileofN-hydroxy-N'-(4-butyl-2-methylphenyl)-formamidine(HET0016),aselectiveinhibitorof20-HETEsynthesis.BiolPharmBull.2005Sep;28(9):1651-4.[2].BorinTF,etal.HET0016decreaseslungmetastasisfrombreastcancerinimmune-competentmousemodel.PLoSOne.2017Jun13;12(6):e0178830.[3].LiuY,etal.TheprotectiveeffectofHET0016onbrainedemaandblood-brainbarrierdysfunctionaftercerebralischemia/reperfusion.BrainRes.2014Jan28;1544:45-53.McePdfHeightCaution:Producthasnotbeenfullyvalidated